相关实验视频

Updated: Jun 29, 2025

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

难溶性药物的相互作用在无形固体分散的溶解中

Marcel Kokott¹, Jörg Breitkreutz¹, Raphael Wiedey¹

¹Institute of Pharmaceutics and Biopharmaceutics, Heinrich Heine University, Duesseldorf Universitaetsstr. 1, Duesseldorf 40225, Germany.

International journal of pharmaceutics: X

|April 8, 2024

概括

开发用于HIV治疗的新型无形固体分散剂 (ASD) 改善了药物溶解. 将洛皮纳维尔与HPMCAS和里托纳维尔与PVPVA结合在一起,比单个聚合物或商业产品提高了性能.

科学领域:

制药科学制药科学
药物输送系统药物输送系统
材料科学材料科学材料科学

背景情况:

固定剂量组合 (FDC) 在艾滋病毒治疗中至关重要,但对配方构成挑战,特别是对于溶性较差的药物.
无形固体分散 (ASD) 是有希望的,但共同配制多种无形药物会增加系统的复杂性.
溶解期间的药物相互作用是发展多种药物ASD的一个重要障碍.

研究的目的:

开发一种新的配方策略,共同配制两种无形抗逆转录病毒药物 - - 里托纳维尔和洛皮纳维尔.
为了克服多药性ASD的溶解挑战和药物相互作用.
通过使用不同的聚合物和聚合物等级来优化溶解配置.

主要方法:

利托纳维尔和洛皮纳维尔的无形固体分散 (ASD) 单独使用热挤出制备.
采用了两种不同的聚合物,聚乙烯-乙烯酸 (PVPVA) 和基甲基纤维素酸 (HPMCAS).
研究了不同等级的HPMCAS来调节药物释放.

主要成果:

使用不同的聚合物用于每个药物的新型配方方法显著提高了溶解性能.
与单独使用PVPVA相比,将洛皮纳维尔嵌入HPMCAS和里托纳维尔嵌入PVPVA显示出更好的溶解.
开发的自闭症障碍者表现优于商业固定剂量组合产品Kaletra®.
在HPMCAS等级的修改允许微调溶解配置文件.

结论:

在ASD中,针对单个药物的不同聚合物的战略选择可以克服多药配方中的溶解挑战.
这种方法为提高固定剂量组合抗逆转录病毒疗法的疗效提供了一个可行的策略.
这些发现为开发复杂药物化合物的先进药物输送系统提供了基础.

关键词:

无形固体的分散性固体.生物相关溶解的溶解固定剂量组合的固定剂量组合.洛皮纳维尔 (Lopinavir) 是一种药物.水溶性较差的药物在水溶性较差的药物里托纳维尔 (Ritonavir) 是一种药物.

更多相关视频

Coherent anti-Stokes Raman Scattering CARS Microscopy Visualizes Pharmaceutical Tablets During Dissolution

Coherent anti-Stokes Raman Scattering CARS Microscopy Visualizes Pharmaceutical Tablets During Dissolution

Published on: July 4, 2014

Formation of Dispersible Taohong Siwu Tablets

Formation of Dispersible Taohong Siwu Tablets

Published on: February 3, 2023

相关概念视频

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...

Factors Influencing Drug Absorption: Drug Dissolution

Factors Influencing Drug Absorption: Drug Dissolution

The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...

Theories of Dissolution: Diffusion Layer Model

Theories of Dissolution: Diffusion Layer Model

Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...